RESUMO
Diabetes remains an important disease worldwide with about 500 million patients globally. In tropical Africa, Morus mesozygia is traditionally used in the treatment of diabetes. Biological and phytochemical investigation of the root bark extracts of the plant led to the isolation of a new prenylated arylbenzofuran named 7-(3-hydroxy-3-methylbutyl)moracin M (1) and two congeners, moracins P (2) and M (3). When compared to acarbose (IC50 = 486 µM), all the isolated compounds are better inhibitors of α-glucosidase with in vitro IC50 values of 16.9, 16.6, and 40.9 µM, respectively. However, they were not active against α-amylase. The compounds also demonstrated moderate inhibition of dipeptidyl peptidase-4 (DPP4). Based on in silico docking studies, all isolates (1, 2, and 3) exhibit binding affinities of -8.7, -9.5, and -8.5 kcal/mol, respectively against α-glucosidase enzyme (PDB: 3AJ7). They are stabilized within the α-glucosidase active site through hydrogen bonds, pi interactions, and hydrophobic interactions. This study provides scientific support for the traditional use of Morus mesozygia in the treatment of diabetes as well as adding to the repository of α-glucosidase inhibitory agents.
RESUMO
The potential of natural and synthetic chalcones as therapeutic leads against different pathological conditions has been investigated for several years, and this class of compounds emerged as a privileged chemotype due to its interesting anti-inflammatory, antimicrobial, antiviral, and anticancer properties. The objective of our study was to contribute to the investigation of this class of natural products as anti-leishmanial agents. We aimed at investigating the structure-activity relationships of the natural chalcone lophirone E, characterized by the presence of benzofuran B-ring, and analogues on anti-leishmania activity. Here we describe an effective synthetic strategy for the preparation of the natural chalcone lophirone E and its application to the synthesis of a small set of chalcones bearing different substitution patterns at both the A and heterocyclic B rings. The resulting compounds were investigated for their activity against Leishmania infantum promastigotes disclosing derivatives 1 and 28a,b as those endowed with the most interesting activities (IC50 = 15.3, 27.2, 15.9 µM, respectively). The synthetic approaches here described and the early SAR investigations highlighted the potential of this class of compounds as antiparasitic hits, making this study worthy of further investigation.
Assuntos
Antiparasitários/química , Antiparasitários/farmacologia , Benzofuranos/química , Biflavonoides/síntese química , Chalconas/síntese química , Indóis/química , Biflavonoides/química , Chalconas/química , Fenômenos Químicos , Técnicas de Química Sintética , Humanos , Leishmania infantum , Estrutura Molecular , Relação Estrutura-AtividadeRESUMO
Alzheimer's disease (AD) is a type of progressive dementia caused by degeneration of the nervous system. A single target drug usually does not work well. Therefore, multi-target drugs are designed and developed so that one drug can specifically bind to multiple targets to ensure clinical effectiveness and reduce toxicity. We synthesised a series of 2-arylbenzofuran derivatives and evaluated their in vitro activities. 2-Arylbenzofuran compounds have good dual cholinesterase inhibitory activity and ß-secretase inhibitory activity. The IC50 value of compound 20 against acetylcholinesterase inhibition (0.086 ± 0.01 µmol·L-1) is similar to donepezil (0.085 ± 0.01 µmol·L-1) and is better than baicalein (0.404 ± 0.04 µmol·L-1). And most of the compounds have good BACE1 inhibitory activity, of which 3 compounds (8, 19 and 20) show better activity than baicalein (0.087 ± 0.03 µmol·L-1). According to experimental results, 2-arylbenzofuran compounds provide an idea for drug design to develop prevention and treatment for AD.
Assuntos
Doença de Alzheimer/tratamento farmacológico , Benzofuranos/uso terapêutico , Nootrópicos/uso terapêutico , HumanosRESUMO
Sophora davidii (Franch.) Skeels is a multi-purpose traditional medicine that has long been used for the treatment of various diseases. To discover the potential bioactive composition of S. davidii, a chemical investigation was thus performed. In this research, two new stilbene oligomers, Davidiol E-F (1-2), one new 4-aryl-substituted isoflavan Davidinin A (3), and one new 2-arylbenzofuran dimer, Shandougenine C (4), as well as six known compounds (5-10) were obtained from the ethyl acetate fraction of Sophora davidii (Franch.) Skeels. The structures of new compounds were established by extensive 1D and 2D nuclear magnetic resonance (NMR) spectra with mass spectroscopy data. The absolute configuration of 1-3 was assigned by comparing its experimental and calculated electronic circular dichroism (ECD) spectra. Compounds 1-10 promoted glucose transporter 4 (GLUT-4) translocations by the range of 1.28-2.60 folds, respectively. Compound 9 showed the most potent glucose transporter 4 translocations with 1.60 fold enhancement. The result attained in this study indicated that the separation and characterization of these compounds plays an important role in the research and development of new anti-diabetic drugs and pharmaceutical industry.
Assuntos
Transportador de Glucose Tipo 4/metabolismo , Raízes de Plantas/química , Sophora/química , Estilbenos/química , Estilbenos/farmacologia , Estrutura Molecular , Transporte Proteico , Estilbenos/análise , Estilbenos/isolamento & purificaçãoRESUMO
In our search for cytotoxic constituents from Vietnamese plants, the methanolic extract of Isotrema tadungense was found to exhibit significant cytotoxic effect. Subsequent phytochemical investigation of ethyl acetate fractions of this plant led to isolation of 11 compounds including one new arylbenzofuran rhamnoside namely aristolochiaside (1), two aristololactams (2 and 3), three lignanamides (4-6) and five phenolic amides (7-11). Their structures were elucidated by 1 D and 2 D NMR and HR-QTOF-MS experiments. Among the isolated compounds, aristolochiaside (1), aristolactam AIIIa (2) and N-trans-sinapoyltyramine (10) exhibited strong and selective cytotoxicity on the HeLa human cancer cell line with IC50 values of 7.59 ± 1.03, 8.51 ± 1.73 and 9.77 ± 1.25 µM, respectively.[Formula: see text].
Assuntos
Antineoplásicos , Amidas , Antineoplásicos/farmacologia , Células HeLa , Humanos , Estrutura Molecular , Extratos VegetaisRESUMO
Two new 2-arylbenzofurans, sesbagrandiflorain D (1) and E (2) along with two known 2-arylbenzofurans, spinosan A (3) and spinosan B (4) were isolated from the stem bark of Sesbania grandiflora L. The structure of two new compounds established by HRESIMS, 1 D NMR (1H, 13C) and 2 D NMR (HMQC, HMBC) spectra. Compounds (1-4) assayed for their cytotoxicity towards three human cancer cells (MCF-7, HeLa, and WiDr). Compound 1 showed very high activity against MCF-7 and WiDr with an IC50 value of 0.06 and 0.60 µg/mL, respectively.
Assuntos
Neoplasias , Sesbania , Humanos , Extratos Vegetais/farmacologiaRESUMO
A new 2-arylbenzofuran, sesbagrandiflorain C (1), together with four known compounds, 2-(3,4-dihydroxy-2-methoxyphenyl)-4-hydroxy-6-methoxybenzofuran-3-carbaldehyde (2), 2-(4-hydroxy-2-methoxyphenyl)-5,6-dimethoxybenzofuran-3-carboxaldehyde (3), sesbagrandiflorain A (4) and sesbagrandiflorain B (5), have been isolated from the stem bark of an Indonesian plant, Sesbania grandiflora (L.) Pers. The chemical structure of compound 1 was elucidated by UV, IR, MS, and NMR spectroscopic techniques. The proton and carbon NMR resonances of 1 were also compared with the predicted chemical shifts obtained from DFT quantum mechanical calculations with Gaussian. None of the compounds showed antibacterial activity against Bacillus subtilis, Escherichia coli, Mycobacterium smegmatis, Pseudomonas aeruginosa, and Staphylococcus aureus in an agar diffusion assay. However, sesbagrandiflorains A (4) and B (5) exhibited moderate activity against Mycobacterium tuberculosis H37Rv. In addition, compounds 1 - 5 have moderate cytotoxicity against HeLa, HepG2, and MCF-7 cancer cell lines.
RESUMO
This study aims to develop new potential therapeutic moracin M prodrugs acting on lung inflammatory disorders. Potential moracin M prodrugs (KW01-KW07) were chemically synthesized to obtain potent orally active derivatives, and their pharmacological activities against lung inflammation were, for the first time, examined in vivo using lipopolysaccharide (LPS)-induced acute lung injury model. In addition, the metabolism of KW02 was also investigated using microsomal stability test and pharmacokinetic study in rats. When orally administered, some of these compounds (30 mg/kg) showed higher inhibitory action against LPSinduced lung inflammation in mice compared to moracin M. Of them, 2-(3,5-bis((dimethylcarbamoyl)oxy)phenyl)benzofuran-6-yl acetate (KW02) showed potent and dose-dependent inhibitory effect on the same animal model of lung inflammation at 1, 3, and 10 mg/kg. This compound at 10 mg/kg also significantly reduced IL-1ß concentration in the bronchoalveolar lavage fluid of the inflamed-lungs. KW02 was rapidly metabolized to 5-(6-hydroxybenzofuran-2-yl)-1,3-phenylene bis(dimethylcarbamate) (KW06) and moracin M when it was incubated with rat serum and liver microsome as expected. When KW02 was administered to rats via intravenous or oral route, KW06 was detected in the serum as a metabolite. Thus, it is concluded that KW02 has potent inhibitory action against LPS-induced lung inflammation. It could behave as a potential prodrug of moracin M to effectively treat lung inflammatory disorders.
RESUMO
A new 2-arylbenzofuran, spathobenzofuran (1), together with ten known compounds including a 2-arylbenzofuran, three pterocarpans and six isoflavones were isolated from the acetone crude extract of the stems of Spatholobus parviflorus. All compounds were characterised by spectroscopic methods. Compound 4 was active (MIC 8 µg/mL) against Gram-negative Pseudomonas aeruginosa TISTR 781 while compound 2 had modest activity against Gram-positive Staphylococcus aureus TISTR 1466 with a MIC value of 16 µg/mL. All isolated compounds showed no cytotoxicity against Vero and KB cells.
Assuntos
Antibacterianos/isolamento & purificação , Citotoxinas/isolamento & purificação , Fabaceae/química , Fenóis/isolamento & purificação , Extratos Vegetais/química , Caules de Planta/química , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Chlorocebus aethiops , Citotoxinas/química , Citotoxinas/farmacologia , Furanos/isolamento & purificação , Humanos , Isoflavonas/isolamento & purificação , Células KB , Testes de Sensibilidade Microbiana , Fenóis/farmacocinética , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Células VeroRESUMO
Black mulberry is a widely acknowledged ancient traditional medicine. Its extract and constituents have been reported to exert various bioactivities including antimicrobial, hypotensive, analgesic etc. effects. While black mulberry preparations are also used as antispasmodic agents in folk medicine, no related studies are available on its isolated constituents. Through an extensive chromatographic purification, seven phenolic compounds were isolated from the methanol extract of Morus nigra root bark, including morusin (1), kuwanon U (2), kuwanon E (3), moracin P (4), moracin O (5), albanol A (6), and albanol B (7). A complete NMR signal assignment of moracin P and O was achieved, and related literature errors confusing the identity of moracin derivatives are hereby clarified. Compounds 2, 5 and 7 were identified as strong antispasmodic agents on isolated rat ileum and tracheal smooth muscles, while compound 3, a methoxy derivative of 2, was inactive. Moracin O (5) inhibited the ileal and tracheal smooth muscle contractions with Emax values of 85% and 302 mg, respectively. Those actions were superior as compared with papaverine. Our findings demonstrate that prenylated arylbenzofurans, geranylated flavonoids and Diels-Alder adducts from Morus nigra are valuable antispasmodic agents. Compounds 2, 5 and 7 are suggested as marker compounds for quality control of antispasmodic mulberry preparations. Moracin O (5) is a new lead compound for related drug development initiatives.
Assuntos
Morus/química , Parassimpatolíticos/química , Fenóis/química , Casca de Planta/química , Extratos Vegetais/química , Raízes de Plantas/química , Benzofuranos/metabolismo , Avaliação Pré-Clínica de Medicamentos , Flavanonas/metabolismo , Metanol/química , Parassimpatolíticos/farmacologia , Prenilação , Resorcinóis/metabolismo , Solventes/química , Relação Estrutura-AtividadeRESUMO
Two new 2-arylbenzofurans, namely 13-O-methyllakoochin B (1) and artogomezianin (2), were isolated from the root bark of Artocarpus gomezianus, along with six known compounds (3-8). The structures of new compounds were determined by spectroscopic and chemical methods. All of the isolates were evaluated for their α-glucosidase inhibitory activity. Artogomezianin (2) and lakoochin A (3) exhibited strong α-glucosidase inhibitory activity with IC50 values of 18.25 and 26.19 µM, respectively, as compared with the positive control acarbose.
Assuntos
Artocarpus/química , Benzofuranos/isolamento & purificação , Benzofuranos/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Casca de Planta/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Benzofuranos/química , Metabolismo dos Carboidratos , Estrutura MolecularRESUMO
Four new prenylated 2-arylbenzofurans, namely artopithecins A-D (1-4), together with five known compounds (5-9) were isolated from the twigs of Artocarpus pithecogallus for the first time. Their structures were elucidated based on extensive spectroscopic analysis and in comparison with literature data. All isolates were evaluated for their inhibitory activities against mushroom tyrosinase. Compounds 3 and 4 displayed significant tyrosinase inhibitory activities with IC50 values of 37.09±0.33 and 38.14±0.21 µM, respectively.
Assuntos
Artocarpus/química , Benzofuranos/farmacologia , Inibidores Enzimáticos/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Caules de Planta/química , Agaricales/enzimologia , Benzofuranos/química , Benzofuranos/isolamento & purificação , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Estrutura Molecular , Monofenol Mono-Oxigenase/metabolismo , Prenilação , Relação Estrutura-AtividadeRESUMO
Native to tropical Asia, Sesbania grandiflora (L.), Pers is a member of the Fabaceae family of flowering plants. All parts of S. grandiflora are used in traditional medicine and phytochemical investigations have been conducted on extracts of the leaves, seeds and roots of S. grandiflora to provide scientific validation of its properties. However, to date, no study has determined the phytochemical constituents of S. grandiflora stem bark. The stem bark powdered of S. grandiflora was extracted exhaustively with n-hexane, EtOAc and 90% aqueous MeOH sequentially. In this study, we successfully isolated two new 2-arylbenzofurans, sesbagrandiflorain A and B, from the EtOAc stem bark of S. grandiflora. The structure elucidation of these compounds was determined by using one- and two-dimensional nuclear magnetic resonance, ultraviolet and infrared spectroscopy and electrospray ionisation time-of-flight mass spectrometry. The finding expands the understanding of the natural constituents of the Fabaceae and, in particular, the Papilionoideae genera.
Assuntos
Benzofuranos/isolamento & purificação , Casca de Planta/química , Sesbania/química , Benzofuranos/química , Indonésia , Estrutura Molecular , Extratos Vegetais/química , Plantas Medicinais/químicaRESUMO
In vitro screening for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the Artocarpus lakoocha root-bark extracts revealed interesting results. Bioassay-guided fractionation resulted in the isolation of two new (1 and 2) and six known 2-arylbenzofurans 3-8, along with one stilbenoid 9 and one flavonoid 10. The structures of the isolated compounds were elucidated by UV, IR, 1D- and 2D-NMR and MS spectroscopic data analysis. Compounds 4, 6 and 7 exhibited more potent AChE inhibitory activity (IC50 = 0.87-1.10 µM) than the reference drug, galantamine. Compounds 4, 8 and 9 displayed greater BChE inhibition than the standard drug. The preferential inhibition of BChE over AChE indicated that 4 also showed a promising dual AChE and BChE inhibitor. The synthetic mono-methylated analogs 4a-c and 6a-b were found to be good BChE inhibitors with IC50 values ranging between 0.31 and 1.11 µM. Based on the docking studies, compounds 4 and 6 are well-fitted in the catalytic triad of AChE. Compounds 4 and 6 showed different binding orientations on BChE, and the most potent BChE inhibitor 4 occupied dual binding to both CAS and PAS more efficiently.
Assuntos
Artocarpus/química , Benzofuranos/química , Benzofuranos/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Éteres Metílicos/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Benzofuranos/metabolismo , Butirilcolinesterase/química , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/metabolismo , Concentração Inibidora 50 , Simulação de Acoplamento Molecular , Conformação ProteicaRESUMO
Chemical investigation of the root bark of Morus alba led to the isolation of a new flavone, dioxycudraflavone A (1) and a new 2-arylbenzofuran, 5-hydroxyethyl moracin M (2), together with seven known compounds namely sanggenon V (3), morusin (4), morusignin L (5), licoflavone C (6), moracin C (7), alfafuran (8) and mulberrofuran G (9). The structure elucidation of these compounds was based on analyses of spectroscopic data including 1D, 2D NMR and HR-ESI-MS. All compounds were evaluated for the α-glucosidase inhibitory and cytotoxic activities. Compounds 2-4, 8 and 9 exhibited strong α-glucosidase inhibitory activities with IC50 less than 10 µM, while only 4 and 9 showed moderate cytotoxic effects against lung cancer cells.
Assuntos
Antineoplásicos/farmacologia , Benzofuranos/farmacologia , Flavonas/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Morus/química , Células A549 , Antineoplásicos/química , Benzofuranos/química , Flavonas/química , Flavonoides/química , Flavonoides/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Casca de Planta/química , Espectrometria de Massas por Ionização por Electrospray , Estilbenos/química , Estilbenos/farmacologia , Terpenos/química , Terpenos/farmacologiaRESUMO
7-hydroxy-5,4'-dimethoxy-2-arylbenzofuran (Ary) is purified from Livistona. It has been demonstrated to have anticancer activity to various tumors in including cervical cancer, but its mechanism is still unclear. In the present, we show that Ary induces cervical cancer cells apoptosis through mitochondria degradation and mediates cervical cancer cell arrest. Further, Ary-inducing cell cycle G1/S-phase arrest is associated with increased cyclin A2 and cyclin dependent kinase 2 (Cdk2) proteins. Knockdown of cyclin A2 using small interfering RNA (siRNA), and inhibiting Cdk2 activity with flavopiridol, strikingly reduced G1/S-phase arrest. Moreover, Ary sustainedly induced phosphorylation of extracellular signal-regulated kinase1/2 (ERK1/2). And ERK1/2 phosphorylation inhibition using specific inhibitor U0126 effectively suppressed cyclin A2 expression, and reduced G1/S-phase arrest induced by Ary. All the experiments in vitro and in vivo verified that Ary has an anticancer effect on cervical cancer. These data provide novel evidences that Ary induces cervical cancer cells apoptosis through mitochondria degradation and cell G1/S-phase arrest. These findings also suggest that ERK-mediated Cdk2/cyclin A signaling pathway is involved in Ary-induced G1/S-phase arrest.
Assuntos
Apoptose/efeitos dos fármacos , Benzofuranos/farmacologia , Ciclina A2/metabolismo , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Proteínas Quinases/metabolismo , Neoplasias do Colo do Útero/tratamento farmacológico , Animais , Benzofuranos/química , Linhagem Celular Tumoral , Quinase 2 Dependente de Ciclina/metabolismo , Feminino , Células HeLa , Humanos , Camundongos Endogâmicos BALB C , Camundongos Nus , Proteína Quinase 1 Ativada por Mitógeno/metabolismo , Proteína Quinase 3 Ativada por Mitógeno/metabolismo , Estrutura Molecular , Fitoterapia/métodos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Carga Tumoral/efeitos dos fármacos , Neoplasias do Colo do Útero/metabolismo , Neoplasias do Colo do Útero/patologia , Ensaios Antitumorais Modelo de Xenoenxerto/métodosRESUMO
The therapeutic effectiveness of moracins as 2-arylbenzofuran derivatives against airway inflammation was examined. Moracin M, O, and R were isolated from the root barks of Morus alba, and they inhibited interleukin (IL)-6 production from IL-1ß-treated lung epithelial cells (A549) at 101-00µM. Among them, moracin M showed the strongest inhibitory effect (IC50=8.1µM). Downregulation of IL-6 expression by moracin M was mediated by interrupting the c-Jun N-terminal kinase (JNK)/c-Jun pathway. Moracin derivatives inhibited inducible nitric oxide synthase (iNOS)-catalyzed NO production from lipopolysaccharide (LPS)-treated alveolar macrophages (MH-S) at 50-100µM. In particular, moracin M inhibited NO production by downregulating iNOS. When orally administered, moracin M (20-60mg/kg) showed comparable inhibitory action with dexamethasone (30mg/kg) against LPS-induced lung inflammation, acute lung injury, in mice with that of dexamethasone (30mg/kg). The action mechanism included interfering with the activation of nuclear transcription factor-κB in inflamed lungs. Therefore, it is concluded that moracin M inhibited airway inflammation in vitro and in vivo, and it has therapeutic potential for treating lung inflammatory disorders.
Assuntos
Anti-Inflamatórios/farmacologia , Benzofuranos/farmacologia , Proteínas Quinases JNK Ativadas por Mitógeno/metabolismo , Pulmão/efeitos dos fármacos , Pulmão/patologia , NF-kappa B/metabolismo , Resorcinóis/farmacologia , Transdução de Sinais/efeitos dos fármacos , Animais , Anti-Inflamatórios/uso terapêutico , Benzofuranos/uso terapêutico , Biocatálise/efeitos dos fármacos , Linhagem Celular Tumoral , Humanos , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inflamação/patologia , Interleucina-1beta/farmacologia , Interleucina-6/biossíntese , Pulmão/metabolismo , Masculino , Camundongos , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/metabolismo , Resorcinóis/uso terapêuticoRESUMO
Detailed phytochemical investigation from the root bark of Morus alba resulted in the isolation of eleven new compounds, including seven 2-arylbenzofuran derivatives (morusalfurans A-G), three flavonoids (morusalnols A-C), and one geranylated stilbene (morusibene A), as well as 22 known compounds. The structures of the identified compounds were elucidated based on a comprehensive analysis of spectroscopic data and Mosher's method. Compounds 2, 3, 6-8, 11, 23, 24, and 29 showed potent inhibition of PL in comparison with the positive control treatment (orlistat, IC50=0.012µM), with IC50 values ranging from 0.09 to 0.92µM.
Assuntos
Inibidores Enzimáticos/farmacologia , Lipase/antagonistas & inibidores , Pâncreas/efeitos dos fármacos , Casca de Planta/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Lipase/metabolismo , Estrutura Molecular , Pâncreas/enzimologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-AtividadeRESUMO
Extracts of Chlorophora regia are frequently used in Ghana in traditional medicine. There is, however, no reported data on the chemical composition of the plant. Comprehensive phytochemical investigation of the stem bark of C. regia resulted in the isolation of three new prenylated 2-arylbenzofuran derivatives, regiafuran A-C (1-3), and one new prenylated flavonol (4), together with fifteen known compounds (5-19). Their structures were elucidated by combined spectroscopic analysis of their NMR and HRESI-MS(n) data. Compounds 1, 2, 5, 9 and 15 exhibited remarkable free radical scavenging properties with IC50 values of 1.9 µg/ml, 2.4 µg/ml, 2.2 µg/ml, 2.1 µg/ml and 1.8 µg/ml, respectively, compared to the standard trolox (IC50 1.1 µg/ml). The isolated compounds did not, however, show any anti-inflammatory potential when tested using a PGE2 (prostaglandin E2) competitive enzyme immunoassay.
Assuntos
Benzofuranos/química , Sequestradores de Radicais Livres/química , Moraceae/química , Casca de Planta/química , Extratos Vegetais/química , Gana , Medicinas Tradicionais Africanas , Estrutura Molecular , PrenilaçãoRESUMO
A new 2-arylbenzofuran compound, 5-dehydroxy-moracin U (1), along with 10 known compounds (2-11), were isolated from cell cultures of Morus alba. Their structures were elucidated on the basis of extensive spectroscopic analyses. The anti-inflammatory activity assay of 1-8 showed that 2 and 8 exhibited significant inhibitory effect on LPS-induced NO production with the values of 76.4% and 98.7% at 10(- 5) M, respectively.